Is tapentadol different from classical opioids?: a review of the evidence
Tapentadol is a single molecule able to deliver analgesia by two distinct mechanisms, a feature which differentiates it from many other analgesics. Pre-clinical data demonstrate two mechanisms of action: mu-opioid receptor agonist activity and noradrenaline re-uptake inhibition. From these, one may...
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| Format: | Article |
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SAGE
2016
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| Online Access: | https://eprints.nottingham.ac.uk/49225/ |
| _version_ | 1848797949545414656 |
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| author | Langford, Richard M. Knaggs, Roger Farquhar-Smith, Paul Dickenson, Anthony H. |
| author_facet | Langford, Richard M. Knaggs, Roger Farquhar-Smith, Paul Dickenson, Anthony H. |
| author_sort | Langford, Richard M. |
| building | Nottingham Research Data Repository |
| collection | Online Access |
| description | Tapentadol is a single molecule able to deliver analgesia by two distinct mechanisms, a feature which differentiates it from many other analgesics. Pre-clinical data demonstrate two mechanisms of action: mu-opioid receptor agonist activity and noradrenaline re-uptake inhibition. From these, one may predict that tapentadol would be applicable across a broad spectrum of pain from nociceptive to neuropathic. The evidence in animal models suggests that norepinephrine re-uptake inhibition (NRI) is a key mechanism and may even predominate over opioid actions in chronic (and especially neuropathic) pain states, reinforcing that tapentadol is different to classical opioids and may, therefore, be an a priori choice for the treatment of neuropathic and mixed pain. The clinical studies and subsequent practice experience and surveillance support the concept of opioid and non-opioid mechanisms of action. The reduced incidence of some of the typical opioid-induced side effects, compared to equianalgesic doses of classical opioids, supports the hypothesis that tapentadol analgesia is only partially mediated by opioid agonist mechanisms. Both the pre-clinical and clinical profiles appear to be differentiated from those of classical opioids. |
| first_indexed | 2025-11-14T20:12:00Z |
| format | Article |
| id | nottingham-49225 |
| institution | University of Nottingham Malaysia Campus |
| institution_category | Local University |
| last_indexed | 2025-11-14T20:12:00Z |
| publishDate | 2016 |
| publisher | SAGE |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | nottingham-492252020-05-04T18:14:07Z https://eprints.nottingham.ac.uk/49225/ Is tapentadol different from classical opioids?: a review of the evidence Langford, Richard M. Knaggs, Roger Farquhar-Smith, Paul Dickenson, Anthony H. Tapentadol is a single molecule able to deliver analgesia by two distinct mechanisms, a feature which differentiates it from many other analgesics. Pre-clinical data demonstrate two mechanisms of action: mu-opioid receptor agonist activity and noradrenaline re-uptake inhibition. From these, one may predict that tapentadol would be applicable across a broad spectrum of pain from nociceptive to neuropathic. The evidence in animal models suggests that norepinephrine re-uptake inhibition (NRI) is a key mechanism and may even predominate over opioid actions in chronic (and especially neuropathic) pain states, reinforcing that tapentadol is different to classical opioids and may, therefore, be an a priori choice for the treatment of neuropathic and mixed pain. The clinical studies and subsequent practice experience and surveillance support the concept of opioid and non-opioid mechanisms of action. The reduced incidence of some of the typical opioid-induced side effects, compared to equianalgesic doses of classical opioids, supports the hypothesis that tapentadol analgesia is only partially mediated by opioid agonist mechanisms. Both the pre-clinical and clinical profiles appear to be differentiated from those of classical opioids. SAGE 2016-11-01 Article PeerReviewed Langford, Richard M., Knaggs, Roger, Farquhar-Smith, Paul and Dickenson, Anthony H. (2016) Is tapentadol different from classical opioids?: a review of the evidence. British Journal of Pain, 10 (4). pp. 217-221. ISSN 2049-4645 Tapentadol opioids pain pharmacology analgesics analgesic mechanisms of action http://journals.sagepub.com/doi/10.1177/2049463716657363 doi:10.1177/2049463716657363 doi:10.1177/2049463716657363 |
| spellingShingle | Tapentadol opioids pain pharmacology analgesics analgesic mechanisms of action Langford, Richard M. Knaggs, Roger Farquhar-Smith, Paul Dickenson, Anthony H. Is tapentadol different from classical opioids?: a review of the evidence |
| title | Is tapentadol different from classical opioids?: a review of the evidence |
| title_full | Is tapentadol different from classical opioids?: a review of the evidence |
| title_fullStr | Is tapentadol different from classical opioids?: a review of the evidence |
| title_full_unstemmed | Is tapentadol different from classical opioids?: a review of the evidence |
| title_short | Is tapentadol different from classical opioids?: a review of the evidence |
| title_sort | is tapentadol different from classical opioids?: a review of the evidence |
| topic | Tapentadol opioids pain pharmacology analgesics analgesic mechanisms of action |
| url | https://eprints.nottingham.ac.uk/49225/ https://eprints.nottingham.ac.uk/49225/ https://eprints.nottingham.ac.uk/49225/ |